Predicted PXR EC50 data for molecules with published -fold activation values obtained from CV-1 cells or Caco-2 cells expressing the human PXR plasmid and a chloramphenicol acetyltransferase reporter plasmid
| Molecule | Catalyst Predicted EC50 | Observed PXR Activation/Deactivation | Reference |
|---|---|---|---|
| μM | |||
| Ecteinascidin | 0.342-a | IC50approx. 3 nM2-b | Synold et al., 2001 |
| Troglitazone | 0.472-a | 7-fold2-b | Jones et al., 2000 |
| LGD1069 (targretin) | 0.572-a | 4-fold | Jones et al., 2000 |
| Nifedipine | 0.582-a | 10-fold2-b | Bertilsson et al., 1998 |
| 5–10-fold | Blumberg et al., 1998 | ||
| Dexamethasone-t-butylacetate | 0.662-a | >5–<10-fold2-b | Lehmann et al., 1998 |
| Docetaxel (Taxotere) | 1.2 | None | Synold et al., 2001 |
| Paclitaxel (Taxol) | 1.4 | EC50 approx. 5 μM | Synold et al., 2001 |
| Lovastatin | 1.5 | ≈5-fold | Lehmann et al., 1998 |
| Phenobarbital | 13 | >17-fold at 1 mM | Jones et al., 2000 |
| ≈5-fold | Lehmann et al., 1998 | ||
| Trans-nonachlor | 5.5 | ≈6-fold | Jones et al., 2000 |
| ≈4-fold | Lehmann et al., 1998 | ||
| Cortisol | 7.1 | ≈3-fold | Bertilsson et al., 1998 |
| ≈4-fold | Blumberg et al., 1998 | ||
| Corticosterone | 8.6 | 12-fold | Blumberg et al., 1998 |
| 3-fold | Jones et al., 2000 | ||
| Hypericin | 3.1 | ≈1.5-fold | Moore et al., 2000a |
| Cholesterol | 4.3 | ≈1.5-fold | Bertilsson et al., 1998 |
| ≈1-fold | Kliewer et al., 1998 | ||
| Progesterone | 5.9 | ≈4-fold | Lehmann et al., 1998 |
| ≈5-fold | Kliewer et al., 1998 | ||
| ≈4-fold | Blumberg et al., 1998 | ||
| Aldosterone | 6.5 | ≈1-fold | Bertilsson et al., 1998 |
| Spironolactone | 6.5 | ≈5-fold | Lehmann et al., 1998 |
| ≈3-fold | Jones et al., 2000 | ||
| ≈3-fold | Blumberg et al., 1998 | ||
| Rutin | 7 | ≈2-fold | Moore et al., 2000a |
| Pregnenolone | 7.4 | ≈3-fold | Bertilsson et al., 1998 |
| ≈5-fold | Lehmann et al., 1998 | ||
| ≈7.5-fold | Kliewer et al., 1998 | ||
| ≈2-fold | Jones et al., 2000 | ||
| ≈3-fold | Blumberg et al., 1998 | ||
| Metyrapone | 9.4 | ≈4-fold | Wright 1999 |
| 17α-Hydroxyprogesterone | 11 | ≈1.5-fold | Jones et al., 2000 |
| Cortisone | 14 | None | Jones et al., 2000 |
| Dihydrotestosterone | 14 | ≈1.5-fold | Jones et al., 2000 |
| ≈5-fold | Blumberg et al., 1998 | ||
| Estradiol | 26 | ≈3-fold | Jones et al., 2000 |
| Scopoletin | 120 | ≈1.5-fold | Moore et al., 2000a |
| Quercetin | 300 | ≈1.5-fold | Moore et al., 2000a |
| Kaempferol | 380 | ≈1-fold | Moore et al., 2000a |
| Myricetin | 15000 | ≈1.5-fold | Moore et al., 2000a |